EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME

EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME

A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherei...

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Hauptverfasser: PASCONE, JOHN, M, STEHLE, NATHAN, W, PARIZA, RICHARD, J, WEIS, SCOT, W, ZIZELMAN, PAUL, VAN ORNUM, SCOTT, G, KUNNEN, KEVIN
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Sprache:eng ; fre ; ger
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CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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creator PASCONE, JOHN, M
STEHLE, NATHAN, W
PARIZA, RICHARD, J
WEIS, SCOT, W
ZIZELMAN, PAUL
VAN ORNUM, SCOTT, G
KUNNEN, KEVIN
description A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).
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In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. 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In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
title EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME
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